雷公藤内酯酮与2,6-二甲基-β-环糊精包合物的制备及性能研究  

Preparation and Properties Study of Inclusion Complex of Triptonide with 2,6-Dimethyl-β-cyclodextrin

作　　者：晋文 李飞杨 黄宇蓉 杨惠文 迟绍明[1] 朱洪友 雷泽 赵焱[1] JIN Wen;LI Fei-Yang;HUANG Yu-Rong;YANG Hui-Wen;CHI Shao-Ming;ZHU Hong-You;LEI Ze;ZHAO Yan(College of Chemistry and Chemical Engineering,Yunnan Normal University,Kunming 650500,China;Guangdong Goodscend Pharmaceutical Technology Co.,Itd,Shantou 515098,China)

机构地区：[1]云南师范大学化学化工学院,昆明650500 [2]广东固升医药科技有限公司,汕头515000

出　　处：《分析化学》2019年第8期1235-1242,共8页Chinese Journal of Analytical Chemistry

基　　金：国家自然科学基金项目(Nos.21362046,21062030);“扬帆计划”引进创新创业团队专项资助项目(No.201312S09)资助~~

摘　　要：通过饱和水溶液法制备了雷公藤内酯酮(TN)和2,6-二甲基-β-环糊精(DM-β-CD)的包合物,采用一维核磁共振氢谱(1H NMR)、二维核磁共振氢谱(2D NMR)、傅里叶变换红外光谱(FT-IR)、X射线衍射(XRD)、扫描电子显微镜(SEM)和热重分析(TG)等技术对TN/DM-β-CD包合物进行表征,推测可能的包合模式。Job曲线法表明,主客体的包合比为1∶1,采用紫外-可见光谱滴定法测定得稳定常数为2891 L/mol。形成包合物后,TN的水溶解度由0.0018 mg/mL增至2.7 mg/mL,提高了150倍。体外释放实验表明,在12 h时包合物累积释放率可达70%,而TN累积释放率达70%需120 h。本研究为制备较高水溶性和低毒性的天然药物活性分子提供了新途径。The inclusion complex of triptonide(TN)and 2,6-dimethyl-β-cyclodextrin(DM-β-CD)was prepared by saturated aqueous solution method.The TN/DM-β-CD inclusion complex was characterized by FTIR,XRD,SEM,and TG,the possible inclusion mode was inferred by 1H NMR and 2D ROESY.The Job's plot showed that the inclusion ratio of host and guest was 1∶1.The stability constant was determined by UV absorbance spectra as 2891 L/mol.The result showed that the DM-β-CD was able to solubilize TN to level as high as 2.7 mg/mL.The water solubility of inclusion complex increased 150 times.In vitro release experiments showed that the cumulative release rate of the inclusion complex reached 70%in 12 h,while the cumulative release rate of TN reached 70%in 120 h.The inclusion complex would have important applications in medical field with higher activity,higher solubility and lower toxicity.

关 键 词：雷公藤内酯酮 2 6-二甲基-β-环糊精 包合物 水溶性 体外释放 

分 类 号：R28[医药卫生—中药学]